Rooks W H, Maloney P J, Shott L D, Schuler M E, Sevelius H, Strosberg A M, Tanenbaum L, Tomolonis A J, Wallach M B, Waterbury D
Drugs Exp Clin Res. 1985;11(8):479-92.
Ketorolac tromethamine[(+/-)-5(benzoyl)-2,3-dihydro-1N-pyrrolizine-1-carboxylic acid tris hydroxymethylaminomethane salt] is a highly potent member of a new class of compounds having analgesic and anti-inflammatory activity. When given orally in tests involving underlying inflammation it was a potent analgesic, whereas it was inactive in tests for narcotic activity. It was also highly active orally in rat models of acute and chronic inflammation and pyresis. These properties are mediated primarily via the compound's potent prostaglandin cyclooxygenase inhibitory activity. The agent elicited mild CNS and cardiovascular activity only at doses far in excess of those required for analgesic and anti-inflammatory activity. A single 10 mg tablet given orally to human volunteers following surgery provided pain relief equivalent to that provided by 10 mg of morphine given intramuscularly. When given intramuscularly to rabbits (0.25 ml of a 0.31-5% solution) or man (3 ml of a 1-3% solution), no drug-related irritation or changes in creatine phosphokinase were seen. Solutions (less than or equal to 0.5%) applied to the eyes of animals and man were not irritating. When applied topically in rat and rabbit models of ocular inflammation, less than or equal to 0.5% solutions of ketorolac tromethamine inhibited the inflammatory response.
酮咯酸氨丁三醇[（±）-5-（苯甲酰基）-2,3-二氢-1H-吡咯嗪-1-羧酸三羟甲基氨基甲烷盐]是一类具有镇痛和抗炎活性的新型化合物中效力很强的一种。在涉及潜在炎症的试验中口服给药时，它是一种强效镇痛药，而在麻醉活性试验中则无活性。在急性和慢性炎症及发热的大鼠模型中口服给药时它也具有高度活性。这些特性主要是通过该化合物强大的前列腺素环氧化酶抑制活性介导的。该药物仅在远远超过镇痛和抗炎活性所需剂量时才会引起轻微的中枢神经系统和心血管活性。术后给人类志愿者口服一片10毫克的片剂，其止痛效果与肌肉注射10毫克吗啡相当。给兔子肌肉注射（0.25毫升0.31-5%的溶液）或给人肌肉注射（3毫升1-3%的溶液）时，未观察到与药物相关的刺激或肌酸磷酸激酶的变化。给动物和人的眼睛滴注浓度小于或等于0.5%的溶液时无刺激性。在大鼠和兔子的眼部炎症模型中局部应用时，浓度小于或等于0.5%的酮咯酸氨丁三醇溶液可抑制炎症反应。
